RU2474586C2 - Эффективные аналоги компстатина - Google Patents
Эффективные аналоги компстатина Download PDFInfo
- Publication number
- RU2474586C2 RU2474586C2 RU2008126232/04A RU2008126232A RU2474586C2 RU 2474586 C2 RU2474586 C2 RU 2474586C2 RU 2008126232/04 A RU2008126232/04 A RU 2008126232/04A RU 2008126232 A RU2008126232 A RU 2008126232A RU 2474586 C2 RU2474586 C2 RU 2474586C2
- Authority
- RU
- Russia
- Prior art keywords
- tryptophan
- peptide
- seq
- trp
- compstatin
- Prior art date
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- RDTRHBCZFDCUPW-KWICJJCGSA-N 2-[(4r,7s,10s,13s,19s,22s,25s,28s,31s,34r)-4-[[(2s,3r)-1-amino-3-hydroxy-1-oxobutan-2-yl]carbamoyl]-34-[[(2s,3s)-2-amino-3-methylpentanoyl]amino]-25-(3-amino-3-oxopropyl)-7-[3-(diaminomethylideneamino)propyl]-10,13-bis(1h-imidazol-5-ylmethyl)-19-(1h-indol Chemical class C([C@H]1C(=O)N[C@@H](CCCNC(N)=N)C(=O)N[C@@H](CSSC[C@@H](C(N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(O)=O)C(=O)N[C@@H](CC=2C3=CC=CC=C3NC=2)C(=O)NCC(=O)N[C@@H](CC=2NC=NC=2)C(=O)N1)C(C)C)C(C)C)=O)NC(=O)[C@@H](N)[C@@H](C)CC)C(=O)N[C@@H]([C@@H](C)O)C(N)=O)C1=CN=CN1 RDTRHBCZFDCUPW-KWICJJCGSA-N 0.000 title description 106
- 108090000765 processed proteins & peptides Proteins 0.000 claims abstract description 190
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- QIVBCDIJIAJPQS-VIFPVBQESA-N L-tryptophane Chemical compound C1=CC=C2C(C[C@H](N)C(O)=O)=CNC2=C1 QIVBCDIJIAJPQS-VIFPVBQESA-N 0.000 claims description 52
- 230000014509 gene expression Effects 0.000 claims description 27
- QIVBCDIJIAJPQS-UHFFFAOYSA-N Tryptophan Natural products C1=CC=C2C(CC(N)C(O)=O)=CNC2=C1 QIVBCDIJIAJPQS-UHFFFAOYSA-N 0.000 claims description 25
- -1 Val Chemical compound 0.000 claims description 22
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- 125000000430 tryptophan group Chemical group [H]N([H])C(C(=O)O*)C([H])([H])C1=C([H])N([H])C2=C([H])C([H])=C([H])C([H])=C12 0.000 claims description 17
- ZADWXFSZEAPBJS-JTQLQIEISA-N 1-methyl-L-tryptophan Chemical compound C1=CC=C2N(C)C=C(C[C@H](N)C(O)=O)C2=C1 ZADWXFSZEAPBJS-JTQLQIEISA-N 0.000 claims description 16
- INPQIVHQSQUEAJ-VIFPVBQESA-N fluorotryptophane Chemical compound C1=C(F)C=C2C(C[C@H](N)C(O)=O)=CNC2=C1 INPQIVHQSQUEAJ-VIFPVBQESA-N 0.000 claims description 16
- ZADWXFSZEAPBJS-UHFFFAOYSA-N racemic N-methyl tryptophan Natural products C1=CC=C2N(C)C=C(CC(N)C(O)=O)C2=C1 ZADWXFSZEAPBJS-UHFFFAOYSA-N 0.000 claims description 15
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 claims description 13
- 150000001413 amino acids Chemical class 0.000 claims description 11
- HUNCSWANZMJLPM-UHFFFAOYSA-N 5-methyltryptophan Chemical compound CC1=CC=C2NC=C(CC(N)C(O)=O)C2=C1 HUNCSWANZMJLPM-UHFFFAOYSA-N 0.000 claims description 9
- AYFVYJQAPQTCCC-GBXIJSLDSA-N L-threonine Chemical compound C[C@@H](O)[C@H](N)C(O)=O AYFVYJQAPQTCCC-GBXIJSLDSA-N 0.000 claims description 9
- 125000003545 alkoxy group Chemical group 0.000 claims description 8
- KRUDZOGZZBVSHD-JTQLQIEISA-N (2s)-2-azaniumyl-3-(1-formylindol-3-yl)propanoate Chemical compound C1=CC=C2C(C[C@H](N)C(O)=O)=CN(C=O)C2=C1 KRUDZOGZZBVSHD-JTQLQIEISA-N 0.000 claims description 7
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- AYFVYJQAPQTCCC-STHAYSLISA-N D-threonine Chemical compound C[C@H](O)[C@@H](N)C(O)=O AYFVYJQAPQTCCC-STHAYSLISA-N 0.000 claims description 5
- DHMQDGOQFOQNFH-UHFFFAOYSA-N Glycine Chemical compound NCC(O)=O DHMQDGOQFOQNFH-UHFFFAOYSA-N 0.000 claims description 5
- KVNPSKDDJARYKK-JTQLQIEISA-N 5-methoxytryptophan Chemical compound COC1=CC=C2NC=C(C[C@H](N)C(O)=O)C2=C1 KVNPSKDDJARYKK-JTQLQIEISA-N 0.000 claims description 4
- KGVHCTWYMPWEGN-FSPLSTOPSA-N Gly-Ile Chemical compound CC[C@H](C)[C@@H](C(O)=O)NC(=O)CN KGVHCTWYMPWEGN-FSPLSTOPSA-N 0.000 claims description 2
- VPZKQTYZIVOJDV-LMVFSUKVSA-N Thr-Ala Chemical compound C[C@@H](O)[C@H](N)C(=O)N[C@@H](C)C(O)=O VPZKQTYZIVOJDV-LMVFSUKVSA-N 0.000 claims description 2
- DFTCYYILCSQGIZ-GCJQMDKQSA-N Thr-Ala-Asn Chemical compound [H]N[C@@H]([C@@H](C)O)C(=O)N[C@@H](C)C(=O)N[C@@H](CC(N)=O)C(O)=O DFTCYYILCSQGIZ-GCJQMDKQSA-N 0.000 claims description 2
- UQTNIFUCMBFWEJ-IWGUZYHVSA-N Thr-Asn Chemical compound C[C@@H](O)[C@H](N)C(=O)N[C@H](C(O)=O)CC(N)=O UQTNIFUCMBFWEJ-IWGUZYHVSA-N 0.000 claims description 2
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| US10125171B2 (en) | 2011-05-11 | 2018-11-13 | Apellis Pharmaceuticals, Inc. | Cell-reactive, long-acting, or targeted compstatin analogs and uses thereof |
| US10308687B2 (en) | 2013-03-15 | 2019-06-04 | Apellis Pharmaceuticals, Inc. | Cell-penetrating compstatin analogs and uses thereof |
| US10407466B2 (en) | 2005-10-08 | 2019-09-10 | Apellis Pharmaceuticals, Inc. | Methods of selecting compstatin mimetics |
| US11040107B2 (en) | 2017-04-07 | 2021-06-22 | Apellis Pharmaceuticals, Inc. | Dosing regimens and related compositions and methods |
| US11338013B2 (en) | 2016-10-17 | 2022-05-24 | Apellis Pharmaceuticals, Inc. | Combination therapy for C3 inhibition |
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Citations (2)
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|---|---|---|---|---|
| WO2004026328A1 (en) * | 2002-09-20 | 2004-04-01 | The Trustees Of The University Of Pennsylvania | Compstatin analogs with improved activity |
| RU2238322C2 (ru) * | 1996-03-07 | 2004-10-20 | Имутран Лимитед | Протеин, обладающий способностью к образованию с3-конвертазы, днк, вектор, конъюгат и их использование |
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| US10407466B2 (en) | 2005-10-08 | 2019-09-10 | Apellis Pharmaceuticals, Inc. | Methods of selecting compstatin mimetics |
| US11001610B2 (en) | 2011-05-11 | 2021-05-11 | Apellis Pharmaceuticals, Inc. | Cell-reactive, long-acting, or targeted compstatin analogs and uses thereof |
| US10125171B2 (en) | 2011-05-11 | 2018-11-13 | Apellis Pharmaceuticals, Inc. | Cell-reactive, long-acting, or targeted compstatin analogs and uses thereof |
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| US11292815B2 (en) | 2012-11-15 | 2022-04-05 | Apellis Pharmaceuticals, Inc. | Cell-reactive, long-acting, or targeted compstatin analogs and related compositions and methods |
| US10875893B2 (en) | 2012-11-15 | 2020-12-29 | Apellis Pharmaceuticals, Inc. | Cell-reactive, long-acting, or targeted compstatin analogs and related compositions and methods |
| RU2705215C2 (ru) * | 2012-11-15 | 2019-11-06 | Апеллис Фармасьютикалс, Инк. | Клеточно-реактивные аналоги компстатина, аналоги компстатина длительного действия или аналоги компстатина нацеленного действия и связанные с ними композиции и способы |
| US10035822B2 (en) | 2012-11-15 | 2018-07-31 | Apellis Pharmaceuticals, Inc. | Cell-reactive, long-acting, or targeted compstatin analogs and related compositions and methods |
| US10941184B2 (en) | 2013-03-15 | 2021-03-09 | Apellis Pharmaceuticals, Inc. | Cell-penetrating compstatin analogs and uses thereof |
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| US11407789B2 (en) | 2013-03-15 | 2022-08-09 | Apellis Pharmaceuticals, Inc. | Cell-penetrating compstatin analogs and uses thereof |
| US11903994B2 (en) | 2015-10-07 | 2024-02-20 | Apellis Pharmaceuticals, Inc. | Dosing regimens |
| US11338013B2 (en) | 2016-10-17 | 2022-05-24 | Apellis Pharmaceuticals, Inc. | Combination therapy for C3 inhibition |
| US11040107B2 (en) | 2017-04-07 | 2021-06-22 | Apellis Pharmaceuticals, Inc. | Dosing regimens and related compositions and methods |
| US11844841B2 (en) | 2017-04-07 | 2023-12-19 | Apellis Pharmaceuticals, Inc. | Dosing regimens and related compositions and methods |
| US11510939B1 (en) | 2019-04-19 | 2022-11-29 | Apellis Pharmaceuticals, Inc. | RNAs for complement inhibition |
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